Assay Detail
Binding
CHEMBL860940
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Inhibition of human CYP11B2 expressed in V79 11B2 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.42 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 9.00 |
| CHEMBL206351 | — | — | 1 | 8.70 |
| CHEMBL206300 | — | — | 1 | 8.40 |
| CHEMBL206550 | — | — | 1 | 8.30 |
| CHEMBL205881 | — | — | 1 | 8.15 |
| CHEMBL206283 | — | — | 1 | 8.15 |
| CHEMBL206070 | — | — | 1 | 7.89 |
| CHEMBL205782 | — | — | 1 | 7.89 |
| CHEMBL205503 | — | — | 1 | 7.52 |
| CHEMBL206273 | — | — | 1 | 7.35 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 7.09 |
| CHEMBL205250 | — | — | 1 | 6.75 |
| CHEMBL208471 | — | — | 1 | 6.48 |
| CHEMBL207751 | — | — | 1 | 6.39 |
| CHEMBL377576 | — | — | 1 | 6.35 |
| CHEMBL206125 | — | — | 1 | 6.13 |
| CHEMBL425054 | — | — | 1 | 5.55 |
| CHEMBL207829 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL206351 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL206300 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL206550 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL205881 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL206283 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL206070 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL205782 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL205503 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL206273 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL205250 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL208471 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL207751 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL377576 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL206125 | — | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL425054 | — | IC50 | = | 2834.0 | nM | 5.55 |
| CHEMBL207829 | — | IC50 | - | — | - |